Article
Biochemistry & Molecular Biology
Toni C. Denner, Niels Heise, Julian Zacharias, Oliver Kraft, Sophie Hoenke, Rene Csuk
Summary: Acetylated triterpenoids were transformed into succinyl-spacered acetazolamide conjugates and tested for their inhibitory actvity on carbonic anhydrase II and cytotoxicity on human tumor cell lines and non-malignant fibroblasts. The conjugates derived from betulin and glycyrrhetinic acid showed the strongest inhibition, while those derived from ursolic or oleanolic acid were weaker inhibitors but had lower cytotoxicity. A betulin-derived conjugate displayed a Ki value of 0.129 μM and an EC50 value of 8.5 μM for human A375 melanoma cells.
Review
Neurosciences
Rebecca Strawbridge, Nefize Yalin, Stelios Orfanos, Allan H. Young
Summary: This scoping review aimed to synthesize all available evidence on the potential effects of acetazolamide on symptoms related to bipolar disorder, acceptability and tolerability, and intervention characteristics. Based on the included studies, most patients responded well to acetazolamide treatment, but the evidence is limited and more clinical trials are needed to validate its efficacy.
Article
Pharmacology & Pharmacy
Hoda E. Teba, Islam A. Khalil, Heba M. El Sorogy
Summary: Acetazolamide is an effective drug for glaucoma treatment, but has systemic side effects. Utilizing cubosomes as a novel nano-delivery system for acetazolamide eye drops can enhance drug permeability and therapeutic efficacy.
Article
Clinical Neurology
Alexey S. Pospelov, Tommi Ala-Kurikka, Samu Kurki, Juha Voipio, Kai Kaila
Summary: Carbonic anhydrase inhibitors effectively block post-asphyxia seizures in neonatal rats by inducing systemic acidosis. These drugs have similar effects on brain pH, suggesting a common mechanism of action in inhibiting seizures. This study provides evidence for the potential safe repurposing of these inhibitors for the treatment of neonatal seizures.
Article
Biochemistry & Molecular Biology
Priti Singh, Parvatha Purnachander Yadav, Baijayantimala Swain, Pavitra S. Thacker, Andrea Angeli, Claudiu T. Supuran, Mohammed Arifuddin
Summary: The study shows that the combination of primary sulfonamide and indolylchalcone can effectively design new compounds with good inhibitory activity against human carbonic anhydrase. These newly synthesized molecules exhibit varying levels of inhibition against different isoforms, with some compounds showing stronger activity against specific isoforms.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Priti Singh, Abhishek Choli, Baijayantimala Swain, Andrea Angeli, Santosh K. Sahoo, Venkata M. Yaddanapudi, Claudiu T. Supuran, Mohammed Arifuddin
Summary: Indole is a widely used structure in drug design and development studies due to its broad bioactivities. Novel urea derivatives of indole with sulfonamide at position-3 were synthesized and found to specifically inhibit human-origin carbonic anhydrase II, with derivative 6l being the most active.
ARCHIV DER PHARMAZIE
(2022)
Article
Biochemistry & Molecular Biology
Toni C. Denner, Andrea Angeli, Marta Ferraroni, Claudiu T. Supuran, Rene Csuk
Summary: Sulfonamides have inhibitory effects on carbonic anhydrases, and sulfonamides with biphenyl- and benzylphenyl substitutions show high selectivity for the treatment of hypoxic cancers and potential applications in treating cerebral edema.
Article
Chemistry, Physical
Sumera Zaib, Imtiaz Khan, Hanan S. Anbar, Seyed-Omar Zaraei, Rawan M. Sbenati, Hafiza Taha Maryam, Hamid Saeed Shah, Mohammed I. El-Gamal
Summary: The present study successfully synthesized a series of indole-picolinamide hybrids as potent inhibitors of bovine carbonic anhydrase II and evaluated their potential as therapeutic targets for neurological disorders, osteoporosis, glaucoma, cancer, and obesity. Compound 1a exhibited strong inhibitory activity and showed potential as an anticancer agent, providing valuable insights for further research.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Toxicology
Francesco P. Busardo, Alfredo F. Lo Faro, Ascanio Sirignano, Raffaele Giorgetti, Jeremy Carlier
Summary: This study aimed to investigate the metabolic fate of acetazolamide (ACZ) in humans. Through in vitro and in vivo experiments, as well as analysis of urine and plasma samples, the metabolites of ACZ and the major metabolic pathways were identified. In contrast to previous studies, this research demonstrated that ACZ is metabolized in humans.
ARCHIVES OF TOXICOLOGY
(2022)
Article
Chemistry, Medicinal
Baijayantimala Swain, Santosh Kumar Sahoo, Priti Singh, Andrea Angeli, Venkata Madhavi Yaddanapudi, Claudiu T. Supuran, Mohammed Arifuddin
Summary: A series of novel sulfonamide containing quinoline compounds were synthesized and tested for their inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. Most of the compounds showed potent inhibitory activity, with some being more effective than the standard drug acetazolamide. 4-substituted benzenesulfonamides exhibited higher potency than 3-substituted derivatives.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Aida Buza, Cuneyt Turkes, Mustafa Arslan, Yeliz Demir, Busra Dincer, Arleta Rifati Nixha, Sukru Beydemir
Summary: Sulfonamides bearing 1,2,3-triazole moiety were designed as inhibitors of human alpha-carbonic anhydrases (hCAs). Some derivatives showed selectivity towards the hCA I and II isoforms. The synthesized compounds demonstrated significant antiproliferative activity and minimal cytotoxicity in various cell lines.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Pharmacology & Pharmacy
Shawn Gulati, Ahmad A. Aref
Summary: This article provides a comprehensive review on the best practices for using acetazolamide in ophthalmic practice, covering its history, mechanism of action, methods of observing efficacy, indications, side effects, allergy information, formulations, dosing, and monitoring. Expert opinion suggests that the benefits of oral carbonic anhydrase inhibitor therapy outweigh the risks in many circumstances, emphasizing the importance of collaboration between eye care practitioners and primary care providers in monitoring and mitigating risks.
EXPERT REVIEW OF CLINICAL PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Andrea Petreni, Viviana De Luca, Andrea Scaloni, Alessio Nocentini, Clemente Capasso, Claudiu T. Supuran
Summary: This study reported an anion and small molecules inhibition study of BteCA iota, proving it to be a zinc(II)-containing enzyme rather than manganese(II)-containing enzyme. The best inhibitors were found to be sulphamic acid, stannate, phenylarsonic acid, among others.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Ecology
David Daniel, Bruno Nunes
Summary: This study assessed the effects of salicylic acid and acetazolamide on the marine gastropod Phorcus lineatus, finding that the species is not sensitive to these pharmaceuticals in terms of specific enzymatic pathways under the adopted conditions.
Review
Biochemistry & Molecular Biology
Mateusz Kciuk, Adrianna Gielecinska, Somdutt Mujwar, Mariusz Mojzych, Beata Marciniak, Rafal Drozda, Renata Kontek
Summary: Carbonic anhydrases IX and CAXII play crucial roles in cancer and have become a focus in anticancer drug design. This offers an opportunity to develop new targeted therapies with fewer side effects.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)